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PE20110676A1 - COMPOUNDS DERIVED FROM ENFUMAFUNGIN WITH ANTIFUNGAL ACTIVITY - Google Patents

COMPOUNDS DERIVED FROM ENFUMAFUNGIN WITH ANTIFUNGAL ACTIVITY

Info

Publication number
PE20110676A1
PE20110676A1 PE2011000156A PE2011000156A PE20110676A1 PE 20110676 A1 PE20110676 A1 PE 20110676A1 PE 2011000156 A PE2011000156 A PE 2011000156A PE 2011000156 A PE2011000156 A PE 2011000156A PE 20110676 A1 PE20110676 A1 PE 20110676A1
Authority
PE
Peru
Prior art keywords
alkyl
enfumafungin
ring
spp
referred
Prior art date
Application number
PE2011000156A
Other languages
Spanish (es)
Inventor
Mark L Greenlee
Robert R Wilkening
James Apgar
Kenneth James Wildonger
Dongfang Meng
Dann L Parker Jr
Original Assignee
Merck Sharp & Dohme
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41669132&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20110676(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of PE20110676A1 publication Critical patent/PE20110676A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/64Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
    • A01N43/647Triazoles; Hydrogenated triazoles
    • A01N43/6531,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008Expansion of ring D by one atom, e.g. D homo steroids

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Agronomy & Crop Science (AREA)
  • Zoology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Engineering & Computer Science (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Environmental Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Cosmetics (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

REFERIDA A UN COMPUESTO DERIVADOS DE ENFUMAFUNGINA DE FORMULA I, DONDE X ES O,H; Re ES C(O)NRfRg, UN GRUPO HETEROARILO ANULAR DE 6 MIEMBROS QUE CONTIENE 1-2 ATOMOS DE N, DONDE HETEROARILO ES, OPCIONALMENTE MONO-SUSTITUIDO EN UN CARBONO DEL ANILLO CON F, Cl, N DEL ANILLO CON O; Rf, Rg, R6 Y R7 SON CADA UNO H, ALQUILO C1-C3; R8 ES ALQUILO C1-C4, CICLOALQUILO C3-C4, CICLOALQUIL-ALQUILO C1-C4; R9 ES METILO, ETILO, ENTRE OTROS. UN COMPUESTO PREFERIDO ES: (1S,4aR, 6aS,7R,8R,10aR,10bR,12aR,14R,15R)-14-[5-(AMINOCARBONIL)-1H-1,2,4-TRIAZOL-1-IL]-8-[(1R)-1,2-DIMETILPROPIL]-15-[[(2R)-2,3-DIMETIL-2-(METILAMINO)BUTIL]OXI]-1,6,6a,7,8,9,10,10a,10b,11,12,12a-DODECAHIDRO-1,6a,8,10a-TETRAMETIL-4H-1,4a-PROPANO-2H-FENANTRO[1,2-c]PIRAN-7-ACIDO CARBOXILICO. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE (1,3)-BETA-DELTA-GLUCAN SINTASA, SIENDO UTILES EN EL TRATAMIENTO DE INFECCIONES FUNGICAS CAUSADAS POR HONGOS Cryptococcus spp, Candida spp O Aspergillus sppREFERRED TO A COMPOUND DERIVED FROM ENFUMAFUNGIN OF FORMULA I, WHERE X IS O, H; Re IS C (O) NRfRg, A 6-MEMBER HETEROARYL RING GROUP CONTAINING 1-2 N ATOMS, WHERE HETEROARYL IS, OPTIONALLY MONO-SUBSTITUTED IN A CARBON OF THE RING WITH F, Cl, N OF THE RING WITH O; Rf, Rg, R6 AND R7 ARE EACH H, C1-C3 ALKYL; R8 IS C1-C4 ALKYL, C3-C4 CYCLOALKYL, C1-C4 CYCLOALKYL ALKYL; R9 IS METHYL, ETHYL, AMONG OTHERS. A PREFERRED COMPOUND IS: (1S, 4aR, 6aS, 7R, 8R, 10aR, 10bR, 12aR, 14R, 15R) -14- [5- (AMINOCARBONYL) -1H-1,2,4-TRIAZOL-1-IL] -8 - [(1R) -1,2-DIMETHYLPROPYL] -15 - [[(2R) -2,3-DIMETHYL-2- (METHYLAMINE) BUTYL] OXY] -1,6,6a, 7,8,9 , 10,10a, 10b, 11,12,12a-DODECAHYDRO-1,6a, 8,10a-TETRAMETHYL-4H-1,4a-PROPANE-2H-PHENANTHRO [1,2-c] PYRAN-7-CARBOXYL ACID. ALSO REFERRED TO A PHARMACEUTICAL COMPOSITION. SAID COMPOUNDS ARE INHIBITORS OF (1,3) -BETA-DELTA-GLUCAN SYNTHASE, BEING USEFUL IN THE TREATMENT OF FUNGIC INFECTIONS CAUSED BY FUNGI Cryptococcus spp, Candida spp OR Aspergillus spp

PE2011000156A 2008-08-12 2009-08-07 COMPOUNDS DERIVED FROM ENFUMAFUNGIN WITH ANTIFUNGAL ACTIVITY PE20110676A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13610608P 2008-08-12 2008-08-12

Publications (1)

Publication Number Publication Date
PE20110676A1 true PE20110676A1 (en) 2011-09-23

Family

ID=41669132

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011000156A PE20110676A1 (en) 2008-08-12 2009-08-07 COMPOUNDS DERIVED FROM ENFUMAFUNGIN WITH ANTIFUNGAL ACTIVITY

Country Status (30)

Country Link
EP (1) EP2326172B1 (en)
KR (1) KR101686075B1 (en)
AR (1) AR073037A1 (en)
BR (1) BRPI0912074B1 (en)
CL (1) CL2011000292A1 (en)
CO (1) CO6351686A2 (en)
CR (1) CR20110075A (en)
DK (1) DK2326172T3 (en)
DO (1) DOP2011000053A (en)
EA (1) EA018337B1 (en)
ES (1) ES2526652T3 (en)
GT (1) GT201100039A (en)
HN (1) HN2011000404A (en)
HR (1) HRP20150009T1 (en)
IL (2) IL210975A (en)
MA (1) MA32628B1 (en)
MX (1) MX2011001656A (en)
MY (1) MY156955A (en)
NI (1) NI201100035A (en)
NZ (1) NZ590914A (en)
PE (1) PE20110676A1 (en)
PL (1) PL2326172T3 (en)
PT (1) PT2326172E (en)
RS (1) RS53731B1 (en)
SI (1) SI2326172T1 (en)
SV (1) SV2011003839A (en)
TW (1) TWI439458B (en)
UA (1) UA105639C2 (en)
WO (1) WO2010019203A1 (en)
ZA (1) ZA201100788B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4039684A1 (en) 2015-01-19 2022-08-10 Scynexis, Inc. Novel salts and polymorphs of scy-078
EA201992413A1 (en) 2017-04-10 2020-03-16 Сайнексис, Инк. ANTI-FOAM AGENTS USED IN COMBINATION
HRP20221414T1 (en) * 2017-08-04 2023-01-20 Scynexis, Inc. Antifungal agents with enhanced activity in acidic ph
MA54866A (en) * 2019-01-30 2022-05-04 Scynexis Inc TRITERPENOID ANTIFUNGALS FOR THE TREATMENT OF FUNGAL OSTEOARTICULAR INFECTIONS
CN113905733A (en) * 2019-05-16 2022-01-07 西尼克斯公司 Antifungal agent such as erebephen herceptin for eliminating candida otic colonization
CN115811989A (en) 2020-05-29 2023-03-17 法国国家科学研究中心 antifungal prodrugs

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2244142C (en) * 1996-01-31 2005-03-29 Merck & Co., Inc. Antifungal compound from hormonema sp.
US5756472A (en) 1996-01-31 1998-05-26 Merck & Co., Inc. Antifungal agent obtained from hormonema
CN1705657A (en) 2002-04-17 2005-12-07 兰贝克赛实验室有限公司 Azole derivatives as antifungal agents
US7863465B2 (en) * 2006-04-03 2011-01-04 Merck Sharp & Dohme Corp. Antifungal agents

Also Published As

Publication number Publication date
BRPI0912074B1 (en) 2021-08-03
RS53731B1 (en) 2015-06-30
PL2326172T3 (en) 2015-03-31
SV2011003839A (en) 2011-07-06
KR101686075B1 (en) 2016-12-13
HRP20150009T1 (en) 2015-02-27
IL210975A0 (en) 2011-04-28
CR20110075A (en) 2011-06-03
HN2011000404A (en) 2013-09-23
MY156955A (en) 2016-04-15
WO2010019203A8 (en) 2011-03-17
EP2326172B1 (en) 2014-10-22
CL2011000292A1 (en) 2011-11-04
EA018337B1 (en) 2013-07-30
NI201100035A (en) 2011-09-20
EP2326172A4 (en) 2012-06-06
TWI439458B (en) 2014-06-01
MA32628B1 (en) 2011-09-01
IL210975A (en) 2015-10-29
UA105639C2 (en) 2014-06-10
ZA201100788B (en) 2012-05-01
WO2010019203A1 (en) 2010-02-18
NZ590914A (en) 2011-11-25
KR20110045054A (en) 2011-05-03
BRPI0912074A2 (en) 2018-10-02
AR073037A1 (en) 2010-10-06
EP2326172A1 (en) 2011-06-01
PT2326172E (en) 2015-02-04
DK2326172T3 (en) 2015-01-26
GT201100039A (en) 2013-08-21
ES2526652T3 (en) 2015-01-14
IL242031A0 (en) 2015-11-30
MX2011001656A (en) 2011-05-25
HK1158017A1 (en) 2012-07-13
DOP2011000053A (en) 2011-04-30
CO6351686A2 (en) 2011-12-20
TW201011004A (en) 2010-03-16
SI2326172T1 (en) 2015-02-27
EA201100350A1 (en) 2011-08-30

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